The 5-HT1B and 5-HT1D agonists in acute migraine therapy: Ergotamine, dihydroergotamine, and the triptans.

Q2 Medicine
Mark Whealy, Werner J Becker
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引用次数: 0

Abstract

The advent of the triptans revolutionized acute migraine treatment. The older migraine-specific drugs, the ergot alkaloids (ergotamine and dihydroergotamine), also relieve migraine attacks through agonism at the 5-HT1B and 5-HT1D receptors, but the triptans have much greater specificity for these receptors. Unlike the ergot alkaloids, the triptans do not activate many other receptor types, and therefore are much better tolerated. This reduction in side effects greatly enhanced their clinical utility as it allowed a far greater proportion of patients to take a full therapeutic dose. As a result, the clinical use of ergotamine is minimal today, although dihydroergotamine still has a significant clinical role. There is extensive evidence that the seven triptans available today, sumatriptan, zolmitriptan, rizatriptan, eletriptan, naratriptan, almotriptan, and frovatriptan, are effective in the acute treatment of migraine. Available formulations include oral tablets, orally dissolving tablets, subcutaneous injections, nasal sprays, and in some countries, rectal suppositories. For optimal benefit, therapy needs to be individualized for a given patient both regarding the triptan chosen and the formulation. This chapter discusses the ergot alkaloids and the triptans, including mechanism of action, evidence for efficacy, clinical use, and adverse effects.

急性偏头痛治疗中的 5-HT1B 和 5-HT1D 激动剂:麦角胺、双氢麦角胺和曲坦类药物。
三苯氧胺的出现彻底改变了急性偏头痛的治疗方法。较早的偏头痛特效药麦角生物碱(麦角胺和双氢麦角胺)也可通过激动5-HT1B和5-HT1D受体缓解偏头痛发作,但三苯氧胺对这些受体的特异性更高。与麦角生物碱不同,三苯氧胺不会激活许多其他类型的受体,因此耐受性更好。副作用的减少大大提高了三苯氧胺的临床实用性,因为这使得更多的患者可以服用足量的治疗剂量。因此,尽管二氢麦角胺仍在临床上发挥着重要作用,但如今麦角胺的临床应用已微乎其微。大量证据表明,目前市面上的七种三普坦(舒马曲坦、佐米曲坦、利扎曲坦、依利曲坦、那拉曲坦、阿莫曲坦和弗罗伐曲坦)对偏头痛的急性期治疗有效。现有制剂包括口服片剂、口腔溶解片剂、皮下注射剂、鼻腔喷雾剂,在一些国家还有直肠栓剂。为了获得最佳疗效,需要根据患者的具体情况选择三苯氧胺和制剂进行个性化治疗。本章讨论麦角生物碱和三苯氧胺,包括作用机制、疗效证据、临床应用和不良反应。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
Handbook of clinical neurology
Handbook of clinical neurology Medicine-Neurology (clinical)
CiteScore
4.10
自引率
0.00%
发文量
302
期刊介绍: The Handbook of Clinical Neurology (HCN) was originally conceived and edited by Pierre Vinken and George Bruyn as a prestigious, multivolume reference work that would cover all the disorders encountered by clinicians and researchers engaged in neurology and allied fields. The first series of the Handbook (Volumes 1-44) was published between 1968 and 1982 and was followed by a second series (Volumes 45-78), guided by the same editors, which concluded in 2002. By that time, the Handbook had come to represent one of the largest scientific works ever published. In 2002, Professors Michael J. Aminoff, François Boller, and Dick F. Swaab took on the responsibility of supervising the third (current) series, the first volumes of which published in 2003. They have designed this series to encompass both clinical neurology and also the basic and clinical neurosciences that are its underpinning. Given the enormity and complexity of the accumulating literature, it is almost impossible to keep abreast of developments in the field, thus providing the raison d''être for the series. The series will thus appeal to clinicians and investigators alike, providing to each an added dimension. Now, more than 140 volumes after it began, the Handbook of Clinical Neurology series has an unparalleled reputation for providing the latest information on fundamental research on the operation of the nervous system in health and disease, comprehensive clinical information on neurological and related disorders, and up-to-date treatment protocols.
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